This invention relates to novel hydroxy-pyrimidine derivatives, more particularly to 2-amino and substituted amino-5-hydroxy-4-methylpyrimidines. This invention is also concerned with a process for the preparation of such novel compounds and with pharmaceutical compositions containing the novel compounds as active ingredients.
United Kingdom Patent Application No. 2045756, published Nov. 5, 1980, discloses 2-isopropylamino-5-hydroxy-pyrimidine as an agent for the treatment of muscular dystrophy. There is no disclosure in this prior application of any 4-methyl analogs.
Chronic gastric and duodenal ulcers, together known as peptic ulcers, are the subject of a variety of treatments, including special diets, drug therapy and surgery, depending upon the severity of the condition. Particularly valuable therapeutic agents useful for the treatment of gastric hyperacidity and peptic ulcers are the histamine-H.sub.2 receptor antagonists, which block the action of the physiologically-active compound histamine at the H.sub.2 -receptor sites in the animal body and thereby inhibit the secretion of gastric acid.
Copending Patent Application Ser. No. 376486 discloses certain 2-guanidino-4-(2-substituted amino-4-imidazolyl)thiazole derivatives as cytoprotective H.sub.2 -antagonists which inhibit ethanol-induced ulcers in rats and thereby have clinical value in the inhibition of gastric ulcers. The cytoprotective H.sub.2 -antagonists or application No. 376486 are prepared from intermediate 2-amino-5-acetylimidazoles and these key intermediates are prepared from 2-amino-5-acetyl oxazole by a rearrangement reaction which is disclosed in application No. 376486.
The 5-hydroxypyrimidine derivatives of the present invention, which are not described per se in application No. 376486, are minor products of the aforesaid rearrangement reaction and the preparation thereof is described in more detail hereinafter.
It has now been found that the novel 5-hydroxypyrimidine derivatives produced as by-products in the general reaction disclosed in application No. 376486, but not isolated or described per se in the disclosure of that application, are valuable therapeutic agents.